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60 Cards in this Set
- Front
- Back
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what is pharmacology
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body of knowledge concerned with the action of chemicals on biologic systems
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what is medical pharmacology
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area of pharmacology concerned with the use of chemicals in the prevention, diagnosis, and treatment of disease especially in humans
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what is toxicology
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area of pharmacology concerned with the undesirable effects of chemicals on biologic systems
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how do drugs vary
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in size from MW 7 (lithium) to over MW 50,000 (thrombolytic enzymes).
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what is MW 7
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lithium
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what is MW 50,000
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thromolytic enzymes
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the majority of drugs have molecular weights between what range
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100-1000
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how to drugs bind to receptors
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chemical bonds
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what are the different types of chemical bonds
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covalent, electrostatic, hydrogen, van del Waals, hydrophobic bonds
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what is a covalent bond
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very strong bond
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what is a electrostatic bond
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weaker than covalent bond
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what bond interactions are weak
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hydrogen, van der Waals, and hydrophobic bonds
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the specifc nature of the drug is of less practical importance than what
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the fact that drugs that bind through weak bonds to their receptors are generally more selective than drugs that bind by means of very strong bonds (b/c weak bonds require a very precise fit of the drug to its receptor if an interaction is to occur)
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weak bonds require what for an interaction to occur
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a very precise fit of the drug to its receptor if an interaction is to occur
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wwhat is permeation
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movement of drug molecules into and within the biologic environment
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what are the different types of permeation
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aqueous diffusion, lipid diffusion, transport by carrier proteins, endocytosis,
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what is aqueous diffusion
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movement of molecules through the watery extracellular and intracellular spaces
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what is lipid diffusion
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Passive movement of molecules across lipid membranes
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Fick's law governs what
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aqueous and lipid diffusion
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Fick's law does not govern what
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transport by special carrier proteins
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what is endocytosis
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occurs through binding to receptors on cell membranes with subsequent internalization by infolding of that area of membrane
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what is Fick's law of diffusion
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Predicts the rate of movement of molecules across a barrier
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what is the formula for Fick's law
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concentration gradient (C1 – C2), and permeability coefficient for the drug and the area and thickness of the barrier are used to compute the rate, as follows:
Rate = (C1 –C2) X Perm coef/Thickness X Area |
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what does Fick's law quantify
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observation that drug absorption is faster from organs with a large surface area and from organs with a thin membrane barrier
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Log is equal to what in the Henderson Hasselbach equations
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pKa-pH
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is log protonated or unporotonated
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either
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weak bases are ionized when
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when they are protonated
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weak acids are not ionized when
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when they are protonated
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when acids are protonated what happens
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they are not ionized
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when bases are protonated what happens
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they are ionized
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what determines the ratio of the protonated to unprotonated form
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pH of the medium
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the pH of the medium determines what
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the ratio of the protonated to unprotonated form
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what are the routes of drug administration
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oral, IV, sub Q, buccal and sublingual, rectal, inhalation, topical, transdermal,
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what are the characteristics of oral administration
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offers convenience, but absorption may be slower and less complete than when parenteral routes are used. Ingested drugs are subject to the first pass effect.
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what are the characteristics of IV administration
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instantaneous and complete absorption. Potentially more dangerous
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what are the characteristics of sub Q administration
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slower absorption than intramuscular route. Avoids first pass metabolism
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what are the characteristics of buccal and sublingual administration
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permits direct absorption into the systemic venous circulation. Avoids first-pass effect
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what are the characteristics of rectal administration
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partial avoidance of first pass effect.
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what are the characteristics of inhalation administration
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Results in rapid absorption. Particularly convenient for drugs that are gases at room temperature
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what are the characteristics of topical administration
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application to skin or mucous membrane for local effect
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what are the characteristics of transdermal administration
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application to the skin for systemic effect
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in regards to absorption what will high blood flow do
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maintains a high drug depot-to-blood concentration gradient and thus maximizes absorption
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in regards to absorption what will concentration changes do
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higher the concentration of the drug at the site of administration, the faster the absorption
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what are the determinants of distribution
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size of organ, blood flow, solubility, binding, metabolism, elimination
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in regards to determinant of distribution what will the size of the organ do
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large organs such as skeletal muscle can take up a large amount of drug because the concentration in the muscle tissue remains low even after large amounts of drug have been transferred
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in regards to determinant of distribution what will blood flow do
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determine rate of uptake. Well perfused tissues will achieve high tissue concentrations rapidly
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in regards to determinant of distribution what will solubility do
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Lipid soluble drugs will distribute rapidly into organs with a high lipid content such as the brain
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in regards to determinant of distribution what will binding do
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binding of a drug to a macro-molecule in a compartment will tend to increase the drug’s concentration in that compartment
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in regards to determinant of distribution what will metabolism do
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terminate action of many drugs before they are excreted by actively metabolizing them to biologically inactive derivatives
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what is inactive as it is administered and must be metabolized in the body to become active
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prodrug
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true or false: Some drugs are not modified by the body; they continue to act until excreted
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true
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true or false: elimination is the same as excretion
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false
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how do elimination and excretion differ
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A drug may be eliminated by metabolism long before the modified molecules are excreted from the body
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what is the first order of elimination
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the rate of elimination is proportionate to the concentration of the drug. The half-life of elimination is constant regardless of the amount of drug in the body
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what is zero elimination
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the rate of elimination is constant regardless of the concentration of the drug
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what can zero elimnation occur with
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ethanol, aspirin, and phenytoin at high doses
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what are the various drug preparations
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solutions and suspensions (syrups, elixirs, parental)
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what is the syrup preparation
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sweetened aqueous solution
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what is the elixir preparation
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sweetened alcoholic solution
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what is the parental preparation
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sterile (IV)
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